1. Cell Cycle/DNA Damage Epigenetics Apoptosis Metabolic Enzyme/Protease Membrane Transporter/Ion Channel
  2. Sirtuin Apoptosis Caspase Lactate Dehydrogenase GLUT
  3. 4'-Bromo-resveratrol

4'-Bromo-resveratrol  (Synonyms: 4′‐BR)

Cat. No.: HY-124113 Purity: 99.94%
Handling Instructions Technical Support

4'-Bromo-resveratrol (4′‐BR) is a dual SIRT1/SIRT3 inhibitor with an IC50 of 0.2 mM for both targets. 4'-Bromo-resveratrol induces caspase-dependent apoptosis, induces G0/G1 cell cycle arrest, and inhiibits proliferation. 4'-Bromo-resveratrol reduces lactate production, glucose uptake, and NAD+/NADH ratio, and downregulates lactate dehydrogenase A and glucose transporter 1 (GLUT1). 4'-Bromo-resveratrol can be used for the research of melanoma.

For research use only. We do not sell to patients.

4'-Bromo-resveratrol

4'-Bromo-resveratrol Chemical Structure

CAS No. : 1224713-90-9

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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Description

4'-Bromo-resveratrol (4′‐BR) is a dual SIRT1/SIRT3 inhibitor with an IC50 of 0.2 mM for both targets. 4'-Bromo-resveratrol induces caspase-dependent apoptosis, induces G0/G1 cell cycle arrest, and inhiibits proliferation. 4'-Bromo-resveratrol reduces lactate production, glucose uptake, and NAD+/NADH ratio, and downregulates lactate dehydrogenase A and glucose transporter 1 (GLUT1). 4'-Bromo-resveratrol can be used for the research of melanoma[1].

IC50 & Target[1]

SIRT1

0.2 mM (IC50)

SIRT3

0.2 mM (IC50)

Caspase 3

 

Caspase 8

 

GLUT1

 

LDHA

 

In Vitro

4'-Bromo-resveratrol (0.0125-0.2 mM; 24-72 h) dose- and time-dependently inhibits proliferation and viability of G361, SK-MEL-28, and SK-MEL-2 human melanoma cells[1].
4'-Bromo-resveratrol (0.0125-0.2 mM; 48 h) dose-dependently impairs clonogenic survival of G361, SK-MEL-28, and SK-MEL-2 human melanoma cells[1].
4'-Bromo-resveratrol (0.0125-0.05 mM; 24-72 h) dose- and time-dependently induces apoptosis in G361, SK-MEL-28, and SK-MEL-2 human melanoma cells, inducing apoptotic morphological changes, including nuclear condensation and fragmentation[1].
4'-Bromo-resveratrol (0.05 mM; 48 h) mediates G0/G1 phase arrest in G361, SK-MEL-28, and SK-MEL-2 human melanoma cells via P21-induced inhibition of Cyclin D1 and CDK6 after 48 hours of treatment[1].
4'-Bromo-resveratrol (0.05 mM; 48 h) reduces expression of glycolysis-related proteins LDHA and GLUT1 in G361, SK-MEL-28, and SK-MEL-2 human melanoma cells after 48 hours of treatment[1].
4'-Bromo-resveratrol (0.05 mM; 48 h) significantly inhibits migration of G361, SK-MEL-28, and SK-MEL-2 human melanoma cells[1].
4'-Bromo-resveratrol (0.025-0.05 mM; 48 h) dose-dependently inhibits aerobic glycolysis in G361, SK-MEL-28, and SK-MEL-2 human melanoma cells, reducing lactate production, glucose uptake, and NAD+/NADH ratio[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: G361, SK-MEL-28, SK-MEL-2 cells
Concentration: 0.0125, 0.025, 0.05, 0.1, 0.2 mM
Incubation Time: 24 h, 48 h, 72 h
Result: Inhibited melanoma cell proliferation and viability in a dose- and time-dependent manner.
Caused massive reduction in proliferation at 0.1 mM and 0.2 mM.
Induced appreciable growth inhibition at 0.025 mM, with statistically significant differences compared to vehicle control.

Apoptosis Analysis[1]

Cell Line: G361, SK-MEL-28, SK-MEL-2
Concentration: 0.0125, 0.025, 0.05 mM
Incubation Time: 24 h, 48 h, 72 h
Result: Increased the percentage of apoptotic cells across all three melanoma cell lines in a dose- and time-dependent manner.
Showed statistically significant differences compared to vehicle control.

Western Blot Analysis[1]

Cell Line: G361, SK-MEL-28, SK-MEL-2
Concentration: 0.05 mM
Incubation Time: 48 h
Result: Decreased protein levels of procaspase-3 and procaspase-8.
Increased levels of cleaved caspase-3.
Induced cleavage of full-length PARP (116 kDa) to its 89 kDa cleaved product.
Significantly diminished expression of PCNA across all three melanoma cell lines.\nAttenuated protein levels of Cyclin D1 and CDK6 across all three melanoma cell lines.
Induced expression of the CDK inhibitor P21 across all three melanoma cell lines.\nSignificantly decreased protein levels of lactate dehydrogenase A (LDHA) across all three melanoma cell lines.
Reduced expression of glucose transporter 1 (GLUT1) across all three melanoma cell lines.

Cell Cycle Analysis[1]

Cell Line: G361, SK-MEL-28, SK-MEL-2
Concentration: 0.05 mM
Incubation Time: 48 h
Result: Caused a significant increase in the percentage of cells in the G0/G1 phase across all three melanoma cell lines.
Induced a concomitant decrease in the G2/M phase population across all three melanoma cell lines.
Showed statistically significant differences compared to vehicle control.
Molecular Weight

291.14

Formula

C14H11BrO2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC1=CC(O)=CC(/C=C/C2=CC=C(C=C2)Br)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (858.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4348 mL 17.1739 mL 34.3477 mL
5 mM 0.6870 mL 3.4348 mL 6.8695 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.4348 mL 17.1739 mL 34.3477 mL 85.8693 mL
5 mM 0.6870 mL 3.4348 mL 6.8695 mL 17.1739 mL
10 mM 0.3435 mL 1.7174 mL 3.4348 mL 8.5869 mL
15 mM 0.2290 mL 1.1449 mL 2.2898 mL 5.7246 mL
20 mM 0.1717 mL 0.8587 mL 1.7174 mL 4.2935 mL
25 mM 0.1374 mL 0.6870 mL 1.3739 mL 3.4348 mL
30 mM 0.1145 mL 0.5725 mL 1.1449 mL 2.8623 mL
40 mM 0.0859 mL 0.4293 mL 0.8587 mL 2.1467 mL
50 mM 0.0687 mL 0.3435 mL 0.6870 mL 1.7174 mL
60 mM 0.0572 mL 0.2862 mL 0.5725 mL 1.4312 mL
80 mM 0.0429 mL 0.2147 mL 0.4293 mL 1.0734 mL
100 mM 0.0343 mL 0.1717 mL 0.3435 mL 0.8587 mL
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4'-Bromo-resveratrol
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